Purity & Documentation

References

LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12-TR binding. Compounds 50, 57 (LIT-927), 65, and 67 are the most potent and soluble cyclic neutraligands identified in vitro and are representative of four novel chemotypes: pyrazoline, pyrimidinone, benzofuranone, and chromanone. LIT-927 is bound to a wide and accessible pocket, which is incompatible with the observed nanomolar binding affinities of our neutraligands[1].

In Vivo

LIT-927 (compound 57) reduces eosinophil recruitment in a murine model of allergic airway hypereosinophilia, LIT-927 is the only one to display inhibitory activity following oral administration. Combined with a high binding selectivity for CXCL12 over other chemokines, LIT-927 represents a powerful pharmacological tool to investigate CXCL12 physiology in vivo and to explore the activity of chemokine neutralization in inflammatory and related diseases[1].

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (38.02 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing Stock Solutions

ConcentrationSolventMass

1 mg

5 mg

10 mg

1 mM

3.0418 mL

15.2091 mL

30.4182 mL

5 mM

0.6084 mL

3.0418 mL

6.0837 mL

10 mM

0.3042 mL

1.5209 mL

3.0418 mL

*Please refer to the solubility information to select the appropriate solvent.